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European Journal of Drug Metabolism and Pharmacokinetics

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https://www.readbyqxmd.com/read/28194579/prediction-of-tissue-to-plasma-ratios-of-basic-compounds-in-mice
#1
Prashant B Nigade, Jayasagar Gundu, K Sreedhara Pai, Kumar V S Nemmani
BACKGROUND: Majority of reported studies so far developed correlation regression equations using the rat muscle-to-plasma drug concentration ratio (Kp-muscle) to predict tissue-to-plasma drug concentration ratios (Kp-tissues). Use of regression equations derived from rat Kp-muscle may not be ideal to predict the mice tissue-Kps as there are species differences. OBJECTIVES: (i) To develop the linear regression equations using mouse tissue-Kps; (ii) to assess the correlation between organ blood flow and/or organ weight with tissue-Kps and (iii) compare the observed tissue-Kps from mice with corresponding predicted tissue-Kps using Richter's rat-Kp specific equations...
February 13, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28185143/characterization-of-1-aminobenzotriazole-and-ketoconazole-as-novel-inhibitors-of-monoamine-oxidase-mao-an-in-vitro-investigation
#2
Abdul Naveed Shaik, Barbara W LeDuc, Ansar A Khan
BACKGROUND AND OBJECTIVES: 1-Aminobenzotriazole, a known time-dependent inhibitor of cytochrome P450 (CYP) enzymes, and ketoconazole, a strong inhibitor of the human CYP3A4 isozyme, are used as standard probe inhibitors to characterize the CYP and/or non-CYP-mediated metabolism of xenobiotics. In the present investigation, 1-Aminobenzotriazole and ketoconazole are characterized as potent monoamine oxidase (MAO) inhibitors in vitro using mouse, rat and human liver microsomes and S9 fractions...
February 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28116646/systemic-bioavailability-and-dose-proportionality-of-omega-3-administered-in-free-fatty-acid-form-compared-with-ethyl-ester-form-results-of-a-phase-1-study-in-healthy-volunteers
#3
Elliot Offman, Michael Davidson, Mohammad Abu-Rashid, Peng Chai, Catarina Nilsson
BACKGROUND: Omega-3 carboxylic acids (OM3-CA) contains eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) in free fatty acid form. Per gram, OM3-CA includes approximately half as much EPA as icosapent ethyl (IPE), an ethyl ester formulation of EPA. OBJECTIVE: The study aim was to assess systemic EPA and EPA + DHA exposures and plasma lipid parameters following multiple OM3-CA or IPE doses under low-fat dietary conditions, and dose proportionality after OM3-CA administration...
January 23, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28078530/evaluation-of-the-population-pharmacokinetic-properties-of-lidocaine-and-its-metabolites-after-long-term-multiple-applications-of-a-lidocaine-plaster-in-post-herpetic-neuralgia-patients
#4
Roberta Bursi, Chiara Piana, Joachim Grevel, Dymphy Huntjens, Irmgard Boesl
BACKGROUND AND OBJECTIVES: Lidocaine 5% medicated plaster is the first lidocaine containing product for chronic use. As no previous investigations have been conducted to evaluate the population pharmacokinetics of long-term exposure to lidocaine 5% medicated plasters, further insights into the evaluation of the pharmacokinetic properties of lidocaine and its metabolites were needed for the assessment of its safety. METHODS: The population pharmacokinetic properties of lidocaine and its metabolites were evaluated after multiple applications of lidocaine 5% medicated plasters based on data collected for up to 14...
January 12, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28070880/on-the-molecular-basis-underlying-the-metabolism-of-tapentadol-through-sulfation
#5
Ahsan F Bairam, Mohammed I Rasool, Katsuhisa Kurogi, Ming-Cheh Liu
BACKGROUND AND OBJECTIVES: Previous studies reported that tapentadol-sulfate represented one of the major metabolites of tapentadol excreted in urine. The current study aimed to identify the human cytosolic sulfotransferases (SULTs) that is(are) capable of sulfating tapentadol and to examine whether human cells and human organ specimens are capable of sulfating tapentadol. METHODS: Thirteen human SULTs, previously expressed and purified, as well as human organ cytosols, were analyzed for tapentadol-sulfating activity using an established sulfotransferase assay...
January 10, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28070879/a-review-of-pharmacogenetics-of-antimalarials-and-associated-clinical-implications
#6
REVIEW
Hazem Elewa, Kyle John Wilby
Genetic variability in drug-metabolizing enzymes and drug transporters is known to influence the pharmacokinetics of many drugs. Antimalarial drugs are a class of agents known to utilize metabolic and elimination pathways prone to genetic variation. This paper aims to review the genetic variants affecting antimalarial medications and discuss their clinical implications. Data were identified for the genes coding for the cytochrome P450 (CYP) enzymes: CYP2C8, CYP2C19, CYP2A6, CYP2D6, CYP2B6, and the P-glycoprotein drug transporter...
January 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28070878/effects-of-caffeic-acid-and-quercetin-on-in-vitro-permeability-metabolism-and-in-vivo-pharmacokinetics-of-melatonin-in-rats-potential-for-herb-drug-interaction
#7
Snehasis Jana, Himanshu Rastogi
BACKGROUND AND OBJECTIVES: Melatonin is a popular dietary supplement and also considered as pharmaceutical product for sleep disorders. Caffeic acid and quercetin are widely distributed in leafy vegetables, fruits, tea extract, and both are used as natural antioxidant. There is an immense concern for health researchers to study the herb/food-drug interactions of melatonin. It is mainly metabolized by CYP1A2 in human so that herbs/foods containing cytochrome P450 (CYP) inhibitors can affect pharmacokinetics of melatonin...
January 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28064419/pharmacokinetics-and-pharmacogenetics-of-carbamazepine-in-children
#8
Natasa Djordjevic, Slobodan M Jankovic, Jasmina R Milovanovic
Although carbamazepine is one of the oldest anticonvulsant drugs, it is still heavily utilized for treatment of epilepsy in children. The aim of this article was to review the current knowledge about pharmacokinetics and pharmacogenetics of carbamazepine in children. The literature for this review was systematically searched for in the MEDLINE and SCINDEKS databases. Oral bioavailability of carbamazepine in children is about 75-85%, and it is approximately 75-85% bound to plasma proteins. Apparent volume of distribution is 1...
January 7, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28064418/novel-antiretroviral-drugs-in-patients-with-renal-impairment-clinical-and-pharmacokinetic-considerations
#9
Dario Cattaneo, Cristina Gervasoni
Highly active antiretroviral therapy (HAART) has dramatically increased the survival of HIV-infected patients from Western countries reducing the incidence of opportunistic infections and AIDS-related malignancies, and improving the patients' quality of life compared with the pre-HAART era. HIV is thus now considered in the West as a chronic disease, with the majority of HIV-infected patients successfully reaching an optimal immune and virological outcome a few months after starting HAART. However, this switch from acute to chronic disease has been accompanied by an increased incidence of chronic kidney disease (CKD), reported in up to 60% of HIV-infected patients...
January 7, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28012025/antifibrotic-effects-of-carvedilol-and-impact-of-liver-fibrosis-on-carvedilol-pharmacokinetics-in-a-rat-model
#10
Ebtehal El-Demerdash, Somaia A Abdel-Sattar, Wesam M El-Bakly, Eman A Mohamed
BACKGROUND AND OBJECTIVES: Carvedilol is a drug of choice in treatment of portal hypertension. The present study was designed to elucidate the potential role of antifibrotic effects of carvedilol in improving hepatic efficiency and the carvedilol oral pharmacokinetic changes during induction of liver fibrosis. METHODS: Rats were given CCl4 (1 ml/kg, intraperitoneal) twice weekly for 6 weeks and/or co-treated with carvedilol (10 mg/kg, orally) three times weekly on alternating days...
December 23, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28000173/in-vitro-evaluation-of-absorption-characteristics-of-peramivir-for-oral-delivery
#11
Ying Li, Zhiyuan Wang, Xin Li, Wei Gong, Xiangyang Xie, Yang Yang, Wu Zhong, Aiping Zheng
BACKGROUND AND OBJECTIVE: Peramivir is a novel antiviral agent approved for the treatment of severe influenza. However, the development of oral formulation of peramivir has been severely hurdled by poor bioavailability (human, ≤3%). The present work aims to evaluate oral permeability characteristics of peramivir. METHODS: In vitro gastrointestinal stability, metabolic stability in human intestinal S9 fraction and Caco-2 permeability were performed. The liquid chromatography with tandem mass spectrometric (LC-MS/MS) was used to quantify peramivir in buffer and biological sample...
December 21, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27928655/in-vivo-pharmacokinetics-of-puerarin-via-different-drug-administration-routes-based-on-middle-cerebral-artery-occlusion-model
#12
Pengyue Li, Jie Bai, Boyu Dong, Yang Lu, Shengwei Zhang, Shuang Guo, Ning Tan, Mengdi Zhao, Shouying Du, Puning Cao
BACKGROUND AND OBJECTIVES: Pueraria labata has traditionally been applied in the treatment of stroke in Chinese clinics. Puerarin is the key ingredient in it for brain protection effect. To find a superior administration route for puerarin in the treatment of ischemic cerebrovascular disease, the pharmacokinetics of puerarin based on the middle cerebral artery occlusion (MCAO) rat via different administration routes were studied and compared. METHODS: Ten rats (MCAO model) divided into two groups were treated with puerarin via intravenous and intranasal routes...
December 7, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27889876/population-pharmacokinetic-pharmacodynamic-modeling-of-5-fluorouracil-for-toxicities-in-rats
#13
Shinji Kobuchi, Yukako Ito, Toshiyuki Sakaeda
BACKGROUND AND OBJECTIVES: Myelosuppression is a dose-limiting toxicity of 5-fluorouracil (5-FU). Predicting the inter- and intra-patient variability in pharmacokinetics and toxicities of 5-FU may contribute to the individualized medicine. This study aimed to establish a population pharmacokinetic-pharmacodynamic model that could evaluate the inter- and intra-individual variability in the plasma 5-FU concentration, 5-FU-induced body weight loss and myelosuppression in rats. METHOD: Plasma 5-FU concentrations, body weight loss, and blood cell counts in rats following the intravenous administration of various doses of 5-FU for 4 days were used to develop the population pharmacokinetic-pharmacodynamic model...
November 26, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28101841/influence-of-sex-and-food-on-the-bioavailability-and-the-r-to-s-conversion-of-ketoprofen-stereoisomers-in-humans
#14
LETTER
Pietro Fagiolino, Nikoletta Fotaki, Marta Vázquez
No abstract text is available yet for this article.
February 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28101840/stereoselective-conversion-of-ketoprofen-in-men-versus-women-from-two-different-oral-dosage-formulations-observations-and-introspection-of-the-pharmacokinetic-data
#15
LETTER
Ranjeet Prasad Dash, Nuggehally R Srinivas
No abstract text is available yet for this article.
February 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27743266/erratum-to-population-pharmacokinetic-modeling-of-oxcarbazepine-active-metabolite-in-chinese-patients-with-epilepsy
#16
Yunli Yu, Quanying Zhang, Wenjun Xu, Chengzhe Lv, Gang Hao
No abstract text is available yet for this article.
February 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27538882/enhancing-oral-absorption-of-%C3%AE-lapachone-progress-till-date
#17
Marival Bermejo, Victor Mangas-Sanjuan, Isabel Gonzalez-Alvarez, Marta Gonzalez-Alvarez
β-Lapachone is a naphthoquinone with high and diverse biological activity. It is useful to treat several pathologies, in particular cancer due to its ability to induce selective apoptosis in tumoral cells. Despite its advantages, β-lapachone's clinical applications are limited by its low solubility in biological fluids and its low specific distribution pattern. In the last decade various formulation strategies have been designed and developed in order to overcome these limitations and to make feasible its wide therapeutic use...
February 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27438788/metabolomics-of-methylphenidate-and-ethylphenidate-implications-in-pharmacological-and-toxicological-effects
#18
Ricardo Jorge Dinis-Oliveira
Methylphenidate (MPH) is primarily indicated for attention-deficit hyperactivity disorder and narcolepsy therapy. A marked individual variability in the dose-response has been observed, and therefore dosage must be titrated for optimal therapeutic effect with minimal toxicity. This variability has been claimed to be predominantly pharmacokinetic. Moreover, due to its similar pharmacodynamics to amphetamine, MPH has been abused and fatalities have been reported. This review aims to discuss metabolomics of MPH, namely by presenting all major and minor metabolites...
February 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27026339/population-pharmacokinetics-modeling-of-inhaled-umeclidinium-for-adult-patients-with-asthma
#19
Shuying Yang, Laurie Lee, Steven Pascoe
BACKGROUND: Umeclidinium (UMEC; a long-acting anti-muscarinic) in combination with fluticasone furoate (an inhaled corticosteroid) is in development for asthma treatment. This secondary analysis aimed to develop a population pharmacokinetic model characterizing UMEC in adults with asthma, and evaluated the impact of covariates on pharmacokinetic parameters. METHODS: Plasma concentration data from study NCT01641692 (assessing once-daily UMEC 15.6, 31.25, 62.5, 125, and 250 mcg, twice daily UMEC 15...
February 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/26994602/pharmacokinetics-of-oral-and-intravenous-oseltamivir-treatment-of-severe-influenza-b-virus-infection-requiring-organ-replacement-therapy
#20
Katharina Karsch, Xi Chen, Oliver Miera, Björn Peters, Patrick Obermeier, Roland C Francis, Válerie Amann, Susanne Duwe, Pieter Fraaij, Alla Heider, Marcel de Zwart, Felix Berger, Albert Osterhaus, Brunhilde Schweiger, Barbara Rath
BACKGROUND AND OBJECTIVES: Patients with severe influenza virus infection, multi-organ failure and organ replacement therapy may absorb and metabolize neuraminidase inhibitors differently. Systematic pharmacokinetic/pharmacodynamic clinical trials are currently lacking in this high-risk group. Inadequate dosing increases the risk of treatment failure and drug resistance, especially in severely ill patients with elevated virus loads. This study aims to explore the impact of organ replacement therapy on oseltamivir drug concentrations...
February 2017: European Journal of Drug Metabolism and Pharmacokinetics
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